WO2019088800A3 - 폴리에틸렌글리콜 유도체 및 이의 제조방법 - Google Patents

폴리에틸렌글리콜 유도체 및 이의 제조방법 Download PDF

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Publication number
WO2019088800A3
WO2019088800A3 PCT/KR2018/013381 KR2018013381W WO2019088800A3 WO 2019088800 A3 WO2019088800 A3 WO 2019088800A3 KR 2018013381 W KR2018013381 W KR 2018013381W WO 2019088800 A3 WO2019088800 A3 WO 2019088800A3
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WIPO (PCT)
Prior art keywords
polyethylene glycol
glycol derivative
preparation
mass production
present
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PCT/KR2018/013381
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English (en)
French (fr)
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WO2019088800A2 (ko
WO2019088800A9 (ko
Inventor
정용규
권보성
곽승환
박은랑
김경도
윤현식
이형우
조영범
Original Assignee
한미정밀화학주식회사
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Priority to US16/648,443 priority Critical patent/US11168180B2/en
Priority to MX2020004332A priority patent/MX2020004332A/es
Priority to BR112020008540-5A priority patent/BR112020008540A2/pt
Priority to JP2020524291A priority patent/JP7258019B2/ja
Priority to EP18872534.5A priority patent/EP3708561B1/en
Priority to AU2018359088A priority patent/AU2018359088A1/en
Priority to CN201880070863.2A priority patent/CN111372911B/zh
Priority to CA3080915A priority patent/CA3080915A1/en
Publication of WO2019088800A2 publication Critical patent/WO2019088800A2/ko
Publication of WO2019088800A9 publication Critical patent/WO2019088800A9/ko
Publication of WO2019088800A3 publication Critical patent/WO2019088800A3/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/76—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings and etherified hydroxy groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
    • C07C217/08—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • C08G65/333—Polymers modified by chemical after-treatment with organic compounds containing nitrogen
    • C08G65/33303—Polymers modified by chemical after-treatment with organic compounds containing nitrogen containing amino group
    • C08G65/33306—Polymers modified by chemical after-treatment with organic compounds containing nitrogen containing amino group acyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/06—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton from hydroxy amines by reactions involving the etherification or esterification of hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/02—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof
    • C07C303/04—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof by substitution of hydrogen atoms by sulfo or halosulfonyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/26—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
    • C07C303/28—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/42—Separation; Purification; Stabilisation; Use of additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/68—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a carbon skeleton substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/75—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing singly-bound oxygen atoms bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C315/00—Preparation of sulfones; Preparation of sulfoxides
    • C07C315/02—Preparation of sulfones; Preparation of sulfoxides by formation of sulfone or sulfoxide groups by oxidation of sulfides, or by formation of sulfone groups by oxidation of sulfoxides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/16—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C317/18—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C41/00—Preparation of ethers; Preparation of compounds having groups, groups or groups
    • C07C41/01—Preparation of ethers
    • C07C41/18—Preparation of ethers by reactions not forming ether-oxygen bonds
    • C07C41/30—Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/03—Ethers having all ether-oxygen atoms bound to acyclic carbon atoms
    • C07C43/04—Saturated ethers
    • C07C43/13—Saturated ethers containing hydroxy or O-metal groups
    • C07C43/135—Saturated ethers containing hydroxy or O-metal groups having more than one ether bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/30—Compounds having groups
    • C07C43/315—Compounds having groups containing oxygen atoms singly bound to carbon atoms not being acetal carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • C08G65/331—Polymers modified by chemical after-treatment with organic compounds containing oxygen
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • C08G65/333—Polymers modified by chemical after-treatment with organic compounds containing nitrogen
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • C08G65/333—Polymers modified by chemical after-treatment with organic compounds containing nitrogen
    • C08G65/33303—Polymers modified by chemical after-treatment with organic compounds containing nitrogen containing amino group
    • C08G65/3331—Polymers modified by chemical after-treatment with organic compounds containing nitrogen containing amino group cyclic
    • C08G65/33313—Polymers modified by chemical after-treatment with organic compounds containing nitrogen containing amino group cyclic aromatic
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    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • C08G65/334—Polymers modified by chemical after-treatment with organic compounds containing sulfur
    • C08G65/3344—Polymers modified by chemical after-treatment with organic compounds containing sulfur containing oxygen in addition to sulfur

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Polyethers (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

본 발명은 폴리에틸렌글리콜 유도체 및 이의 제조방법에 관한 것으로서, 본 발명에 따른 폴리에틸렌글리콜 유도체의 제조공정은 의약품 링커로 다양하게 활용할 수 있는 신규한 폴리에틸렌글리콜 유도체를 제공할 수 있고, 대량 생산에 적합하고 효율적이며 고품질의 제품을 재현성있게 대량생산할 수 있는 장점이 있다.
PCT/KR2018/013381 2017-11-06 2018-11-06 폴리에틸렌글리콜 유도체 및 이의 제조방법 WO2019088800A2 (ko)

Priority Applications (8)

Application Number Priority Date Filing Date Title
US16/648,443 US11168180B2 (en) 2017-11-06 2018-11-06 Polyethylene glycol derivative and preparation method thereof
MX2020004332A MX2020004332A (es) 2017-11-06 2018-11-06 Derivado de polietilenglicol y metodo de preparacion del mismo.
BR112020008540-5A BR112020008540A2 (pt) 2017-11-06 2018-11-06 derivado de polietilenoglicol e método de preparação deste
JP2020524291A JP7258019B2 (ja) 2017-11-06 2018-11-06 ポリエチレングリコール誘導体及びこの製造方法
EP18872534.5A EP3708561B1 (en) 2017-11-06 2018-11-06 Polyethylene glycol derivative and preparation method thereof
AU2018359088A AU2018359088A1 (en) 2017-11-06 2018-11-06 Polyethylene glycol derivative and preparation method thereof
CN201880070863.2A CN111372911B (zh) 2017-11-06 2018-11-06 聚乙二醇衍生物及其制备方法
CA3080915A CA3080915A1 (en) 2017-11-06 2018-11-06 Polyethylene glycol derivative and preparation method thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2017-0146940 2017-11-06
KR20170146940 2017-11-06

Publications (3)

Publication Number Publication Date
WO2019088800A2 WO2019088800A2 (ko) 2019-05-09
WO2019088800A9 WO2019088800A9 (ko) 2019-06-13
WO2019088800A3 true WO2019088800A3 (ko) 2019-08-01

Family

ID=66332612

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PCT/KR2018/013381 WO2019088800A2 (ko) 2017-11-06 2018-11-06 폴리에틸렌글리콜 유도체 및 이의 제조방법

Country Status (10)

Country Link
US (1) US11168180B2 (ko)
EP (1) EP3708561B1 (ko)
JP (1) JP7258019B2 (ko)
KR (1) KR102353479B1 (ko)
CN (1) CN111372911B (ko)
AU (1) AU2018359088A1 (ko)
BR (1) BR112020008540A2 (ko)
CA (1) CA3080915A1 (ko)
MX (1) MX2020004332A (ko)
WO (1) WO2019088800A2 (ko)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114524943B (zh) * 2022-04-22 2022-09-16 天津凯莱英制药有限公司 聚乙二醇-甘油衍生物及其中间体各自的制备方法

Citations (4)

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JP2011084632A (ja) * 2009-10-14 2011-04-28 Senka Pharmacy:Kk ポリエチレングリコールの誘導体およびそれを有効成分として含む抗腫瘍剤
US20120004423A1 (en) * 2008-12-22 2012-01-05 Ge Healthcare Limited Synthesis of obtaining modified polyethylene glycol intermediates
WO2017002853A1 (ja) * 2015-06-30 2017-01-05 株式会社東北テクノアーチ ヘテロ型単分散ポリエチレングリコール、ヘテロ型単分散ポリエチレングリコール製造用中間体及びそれらの製造方法、並びに、ヘテロ型単分散ポリエチレングリコール結合体
KR20170104409A (ko) * 2016-03-07 2017-09-15 한미약품 주식회사 폴리에틸렌 글리콜 유도체 및 이의 용도

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KR20120134158A (ko) 2004-03-17 2012-12-11 안티캔서, 인코포레이티드 폴리에틸렌 글리콜(ｐｅｇ) 단백질 결합을 증가시키기 위한 방법
EP1857462B9 (en) * 2005-02-18 2013-02-13 Nof Corporation Polyoxyalkylene derivative
JP5515224B2 (ja) * 2007-02-28 2014-06-11 日油株式会社 多分岐鎖ポリオキシアルキレン誘導体

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US20120004423A1 (en) * 2008-12-22 2012-01-05 Ge Healthcare Limited Synthesis of obtaining modified polyethylene glycol intermediates
JP2011084632A (ja) * 2009-10-14 2011-04-28 Senka Pharmacy:Kk ポリエチレングリコールの誘導体およびそれを有効成分として含む抗腫瘍剤
WO2017002853A1 (ja) * 2015-06-30 2017-01-05 株式会社東北テクノアーチ ヘテロ型単分散ポリエチレングリコール、ヘテロ型単分散ポリエチレングリコール製造用中間体及びそれらの製造方法、並びに、ヘテロ型単分散ポリエチレングリコール結合体
KR20170104409A (ko) * 2016-03-07 2017-09-15 한미약품 주식회사 폴리에틸렌 글리콜 유도체 및 이의 용도

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Title
OBA, M. ET AL.: "Cyclic RGD Peptide-Conjugated Polyplex Micelles as a Targetable Gene Delivery System Directed to Cells Possessing α v β 3 and α v β 5 Integrins", BIOCONJUGATE CHEM., vol. 18, 2007, pages 1415 - 1423, XP055631043 *

Also Published As

Publication number Publication date
US20200231749A1 (en) 2020-07-23
EP3708561A4 (en) 2021-11-03
BR112020008540A2 (pt) 2020-10-06
EP3708561B1 (en) 2024-05-08
WO2019088800A2 (ko) 2019-05-09
KR102353479B1 (ko) 2022-01-21
US11168180B2 (en) 2021-11-09
JP2021501816A (ja) 2021-01-21
AU2018359088A1 (en) 2020-05-21
CA3080915A1 (en) 2019-05-09
CN111372911A (zh) 2020-07-03
JP7258019B2 (ja) 2023-04-14
KR20190051856A (ko) 2019-05-15
CN111372911B (zh) 2023-06-13
MX2020004332A (es) 2020-08-03
WO2019088800A9 (ko) 2019-06-13
EP3708561A2 (en) 2020-09-16

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